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(1S,3S)-3-acetyl-3,5,10-trihydroxy-6,11-dioxo-1,2,3,4,6,11-hexahydrotetracen-1-yl 3-amino-2,3,6-trideoxy-alpha-L-lyxo-hexopyranoside
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-
(2-hydroxyphenyl)(4-hydroxyphenyl)methanone
50.7% inhibition at 0.1 mM
(3S)-3,5,12-trihydroxy-3-(hydroxyacetyl)-10-methoxy-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl 3-(2-cyanopiperidin-1-yl)-2,3,6-trideoxy-alpha-D-glycero-hexopyranoside
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-
(3S)-3,5,12-trihydroxy-3-(hydroxyacetyl)-10-methoxy-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl-2,6-dideoxy-beta-L-threo-hexopyranoside
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-
(3S)-3,5,12-trihydroxy-3-(hydroxyacetyl)-10-methoxy-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl-3-amino-2,3,6-trideoxy-alpha-D-erythro-hexopyranoside
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-
(3S)-3,5,12-trihydroxy-3-(hydroxyacetyl)-10-methoxy-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl-3-amino-2,3,6-trideoxy-beta-L-threo-hexopyranoside
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-
(3S)-3,5,12-trihydroxy-3-(hydroxyacetyl)-10-methoxy-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl-4-amino-2,4,6-trideoxy-alpha-D-erythro-hexopyranoside
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-
(3S)-3,5,12-trihydroxy-3-(hydroxyacetyl)-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl-2,6-dideoxy-beta-L-threo-hexopyranoside
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(3S)-3,5,12-trihydroxy-3-(hydroxyacetyl)-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl-3-amino-2,3,6-trideoxy-alpha-D-erythro-hexopyranoside
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-
(3S)-3-acetyl-3,5,10-trihydroxy-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl-3-amino-2,3,6-trideoxy-alpha-D-erythro-hexopyranoside
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-
(3S)-3-acetyl-3,5,12-trihydroxy-10-methoxy-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl-3,4-diamino-2,3,4,6-tetradeoxy-alpha-D-erythro-hexopyranoside
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-
(3S)-3-acetyl-3,5,12-trihydroxy-10-methoxy-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl-3-amino-2,3,6-trideoxy-alpha-D-erythro-hexopyranoside
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-
(3S)-3-acetyl-3,5,12-trihydroxy-10-methoxy-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl-4-amino-2,4,6-trideoxy-alpha-D-threo-hexopyranoside
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-
(3S)-3-acetyl-3,5,12-trihydroxy-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl-2,6-dideoxy-beta-L-threo-hexopyranoside
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-
(3S)-3-acetyl-3,5,12-trihydroxy-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl-3-amino-2,3,6-trideoxy-alpha-D-erythro-hexopyranoside
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-
(7R,9R)-idarubicin
Tequatrovirus T4
-
-
(8S)-10-[[(2R,4R)-4-amino-6-methyltetrahydro-2H-pyran-2-yl]oxy]-6,8,11-trihydroxy-8-(hydroxyacetyl)-1-methoxy-5a,7,8,9,10,11a-hexahydrotetracene-5,12-dione
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-
(8S)-10-[[(2S,4S,5S)-4-amino-5-iodo-6-methyltetrahydro-2H-pyran-2-yl]oxy]-6,8,11-trihydroxy-8-(hydroxyacetyl)-1-methoxy-5a,7,8,9,10,11a-hexahydrotetracene-5,12-dione
-
-
(8S)-8-acetyl-10-[[(2R,4R)-4-amino-6-methyltetrahydro-2H-pyran-2-yl]oxy]-6,8,11-trihydroxy-1-methoxy-5a,7,8,9,10,11a-hexahydrotetracene-5,12-dione
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-
(9S)-7-[[(2R,4R)-4-amino-6-methyltetrahydro-2H-pyran-2-yl]oxy]-6,9,11-trihydroxy-9-(hydroxyacetyl)-5a,7,8,9,10,11a-hexahydrotetracene-5,12-dione
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-
(9S)-9-acetyl-7-[[(2S,5R)-5-amino-6-methyltetrahydro-2H-pyran-2-yl]oxy]-6,9,11-trihydroxy-5a,7,8,9,10,11a-hexahydrotetracene-5,12-dione
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-
(E)-2-(3,5-dibromo-4-methylphenylamino)-N'-(2-hydroxy-5-nitrobenzylidene)acetohydrazide
-
inhibits Lig1 and Lig3
12-(6-piperidin-1-ylhexyl)-7,12-dihydro-6H-[1]benzothiepino[5,4-b]indole
-
-
2,3-dioxo-2,3-dihydro-1H-indole-7-carboxylic acid
59.3% inhibition at 0.1 mM
2-[(3,5-dibromo-4-methylphenyl)amino]-N'-[(1E)-(2-hydroxy-5-nitrophenyl)methylidene]acetohydrazide
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-
2-[(3,5-dibromo-4-methylphenyl)amino]-N'-[(1Z)-(2-hydroxy-5-nitrophenyl)methylidene]acetohydrazide
78.3% inhibition at 0.1 mM
3-amino-2-[[(1E)-phenylmethylidene]amino]-5-sulfanylphenol
68.8% inhibition at 0.1 mM
3-[(4-bromophenyl)sulfonyl]-N-[2-(4-sulfamoylphenyl)ethyl]propanamide
53.4% inhibition at 0.1 mM
4',6-Diamidino-2-phenylindole
Tequatrovirus T4
-
-
4-([[(4-carboxy-5-methylfuran-2-yl)methyl]sulfanyl]methyl)-5-methylfuran-2-carboxylic acid
91% inhibition at 0.1 mM
4-chloro-5-[(2E)-2-(4-hydroxy-3-nitrobenzylidene)hydrazinyl]pyridazin-3(2H)-one
-
specific for Lig1
4-chloro-5-[(2E)-2-[(4-hydroxy-3-nitrophenyl)methylidene]hydrazino]pyridazin-3(2H)-one
-
-
4-chloro-5-[(2Z)-2-[(4-hydroxy-3-nitrophenyl)methylidene]hydrazino]pyridazin-3(2H)-one
59.8% inhibition at 0.1 mM
4-demethyl-6-deoxydaunorubicin
-
-
5-(methylsulfanyl)thiophene-2-carboxylic acid
60.5% inhibition at 0.1 mM
6-amino-5-[[(1E)-phenylmethylidene]amino]-2-sulfanylpyrimidin-4-ol
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-
7-(4-methoxyphenyl)pteridine-2,4-diol
52.5% inhibition at 0.1 mM
9-beta-D-Arabinofuranosyl-2-fluoroadenine triphosphate
-
0.08 mM, 90% inhibition
ADP
-
inhibits catalysis of nick-sealing by the ligase-AMP intermediate
ammonium sulfate
10 mM, 60% inhibition
Anthracycline derivatives
apurine/apyrimidinic endonuclease I
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inhibition if the DNA ligase I substrate has a tetrahydrofuran residue on the 5'-downstream primer of a nick, simulating a reduced abasic site
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Arabinosyl-2-fluoro-ATP
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-
Cd2+
-
5 mM, abolishes ligation reaction in presence of 5 mM Mg2+
CdCl2
-
0.04 mM, complete inhibition
Co2+
-
5 mM, abolishes ligation reaction in presence of 5 mM Mg2+
CTP
-
2 mM, 18% inhibition of single-turnover ligation
Cu2+
-
partially inhibitory, ligation activity in presence of Mg2+
GTP
-
2 mM, 38% inhibition of single-turnover ligation
N-[5-([5-[(3-amino-3-iminopropyl)carbamoyl]-1-methyl-1H-pyrrol-3-yl]carbamoyl)-1-methyl-1H-pyrrol-3-yl]-4-(formylamino)-1-methyl-1H-pyrrole-2-carboxamide hydrochloride
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distamycin A
N-[5-([5-[(3-amino-3-iminopropyl)carbamoyl]-1-methyl-1H-pyrrol-3-yl]carbamoyl)-1-methyl-1H-pyrrol-3-yl]-4-[([4-[bis(2-chloroethyl)amino]phenyl]carbonyl)amino]-1-methyl-1H-pyrrole-2-carboxamide hydrochloride
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FCE-24517
NH4Cl
100 mM, approximately 70% inhibition
Ni2+
-
5 mM, abolishes ligation reaction in presence of 5 mM Mg2+
p-chloromercuribenzoate
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-
PCNA
inhibition of the DNA ligase I activity by proliferating cell nuclear antigen, PCNA, complexes StoPCNA. StoPCNA1 and StoPCNA3, overview
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Protolichesterinic acid
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Replication factor C
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LigI interacts with and is inhibited by replication factor C
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sanguinarine
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low active inhibitor
spermine
Tequatrovirus T4
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-
UTP
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2 mM, 7% inhibition of single-turnover ligation
Zn2+
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5 mM, abolishes ligation reaction in presence of 5 mM Mg2+
ZnCl2
-
0.8 mM, complete inhibition
[(7-chloro-4-nitro-2,1,3-benzoxadiazol-5-yl)sulfanyl]acetic acid
60.6% inhibition at 0.1 mM
actinomycin
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-
AMPPNP
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nonhydrolyzable ATP analogue
AMPPNP
Tequatrovirus T4
-
no inhibition
Anthracycline derivatives
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inhibit human DNA ligase I and rat DNA ligase I and III in the poly[d(A-T)] joining assay
Anthracycline derivatives
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the inhibitors possessing a 3'-amino-4'-deoxy-sugar carrying no other modifications exhibit the most potent inhibition
Anthracycline derivatives
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inhibit human DNA ligase I and rat DNA ligase I and III in the poly[d(A-T)] joining assay
ATP
-
2 mM 50% inhibition
ATP
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inhibits the last step of the reaction, which involves cleavage of the diphosphate bond of the DNA-adenylate intermediate and phosphodiester bond formation
ATP
Tequatrovirus T4
-
5 mM and higher. 5 mM, completely inhibits blunt end ligation, only 8% reduces ligation of cohesive DNA ends
Ca2+
-
CaCl2 inhibits Mg2+-catalyzed reaction
Ca2+
-
partially inhibitory, ligation activity in presence of Mg2+
Ca2+
-
inhibition above 40 mM
chelerythrine chloride
-
-
chelerythrine chloride
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low active inhibitor
Cs+
Tequatrovirus T4
-
-
Cs+
Tequatrovirus T4
-
0.2 M
dATP
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competitive with respect to ATP
dATP
Tequatrovirus T4
-
competitive with respect to ATP
dATP
Tequatrovirus T4
-
-
Distamycin
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and derivatives, inhibit human DNA ligase I and rat DNA ligase I and III in the poly[d(A-T)] joining assay
Distamycin
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and derivatives, inhibit human DNA ligase I and rat DNA ligase I and III in the poly[d(A-T)] joining assay
doxorubicin
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an antitumor drug, potent inhibitor
doxorubicin
Tequatrovirus T4
-
-
EDTA
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-
EDTA
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EDTA rapidly inactivates all LIG1-catalyzed reactions
Ethidium bromide
-
-
Ethidium bromide
Tequatrovirus T4
-
-
Fagaronine chloride
-
-
Fagaronine chloride
-
most potent inhibitor
K+
-
50 mM, 50% inhibition
K+
Tequatrovirus T4
-
0.2 M
K+
Tequatrovirus T4
-
extent of inhibition varies with the terminal sequence of the duplex DNA used as substrate
KCl
100 mM, approximately 70% inhibition
KCl
50 mM, 70% inhibition
KCl
-
30 mM, more than 60% reduction in product formation
KCl
100 mM, 85% inhibition, not inhibited below 50 mM
Li+
Tequatrovirus T4
-
-
Li+
Tequatrovirus T4
-
0.2 M
Mn2+
-
MnCl2 inhibits Mg2+-catalyzed reaction
Mn2+
-
5 mM, abolishes ligation reaction in presence of 5 mM Mg2+
Na+
Tequatrovirus T4
-
-
Na+
Tequatrovirus T4
-
0.2 M
Na+
Tequatrovirus T4
-
extent of inhibition varies with the terminal sequence of the duplex DNA used as substrate. Resistance to inhibition in the order from strong to weak: HindIII, PstI, EcoRI, BamHI, SalI in cohesive end ligation, and EcoRV, ScaI, PvuII, NruI in blunt end ligation
NaCl
100 mM, approximately 70% inhibition
NaCl
complete inhibition at above 200 mM
NaCl
50 mM, 75% inhibition, 80 mM, 90% inhibition
NaCl
-
above 20 mM, more than 60% reduction in product formation
NaCl
NaCl concentrations above 100 mM have an inhibitory effect
NaCl
100 mM, 85% inhibition, not inhibited below 50 mM
NEM
-
-
NEM
-
concentrations higher than 1 mM
NH4+
Tequatrovirus T4
-
-
NH4+
Tequatrovirus T4
-
0.2 M
Nitidine chloride
-
-
Nitidine chloride
-
most potent inhibitor
phosphate
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wild type enzyme activity is reduced by 4%, 35%, 73%, and 91% at 100 mM, 150 mM, 200 mM, and 250 mM phosphate, respectively
phosphate
Tequatrovirus T4
-
inhibits blunt end ligation
Protein inhibitor
-
inhibitor protein purified from human cells, MW 55000-75000, forms a reversible complex with DNA ligase I, but has no effect on DNA ligase II. The inhibitor may play a regulatory role for DNA replication and repair
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Protein inhibitor
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specific inhibitor for DNA ligase I , this protein inhibitor may play a specific role in regulating DNA ligation during replication, repair, or recombination
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pyridoxal 5'-phosphate
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DNA ligase I
pyridoxal 5'-phosphate
-
inhibits last step of the reaction, which involves cleavage of the diphosphate bond of the DNA-adenylate intermediate and phosphodiester bond formation
spermidine
Tequatrovirus T4
-
-
spermidine
Tequatrovirus T4
-
10 mM, inhibits joining of DNA blunt ends, no effect on the joining of cohesive termini
Swertifrancheside
-
-
Swertifrancheside
-
flavonoxanthone glucoside
additional information
-
not inhibited by 2,4-diamino-7-dimethylamino-pyrimido[4,5-d]pyrimidine, trimethoprim, and methotrexate
-
additional information
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not inhibited by apigenin, betulinic acid, (-)-catechin, chloroquine, chelidonine, N-demethylfagaronine, berberine, coptisine chloride, tetrahydroberberine, and tertahydropalmatine
-
additional information
-
dephosphorylation causes drastic reduction in enzyme activity
-
additional information
the effects of mismatches on joining short oligonucleotides by Methanocaldococcus jannaschii DNA ligase are fully characterized. The mismatches at the first position 5' to the nick inhibits ligation more than those at the first position 3' to the nick. The mismatches at other positions 5' to the nick (3rd to 7th sites) exhibits less inhibition on ligation. However, the introduction of a C/C mismatch at the third position 5' to the nick completely inhibits the ligation of the terminal-mismatched nick of an oligonucleotide duplex by the DNA ligase
-
additional information
-
the effects of mismatches on joining short oligonucleotides by Methanocaldococcus jannaschii DNA ligase are fully characterized. The mismatches at the first position 5' to the nick inhibits ligation more than those at the first position 3' to the nick. The mismatches at other positions 5' to the nick (3rd to 7th sites) exhibits less inhibition on ligation. However, the introduction of a C/C mismatch at the third position 5' to the nick completely inhibits the ligation of the terminal-mismatched nick of an oligonucleotide duplex by the DNA ligase
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additional information
no inhibition with ATP concentrations up to 0.5 mM
-
additional information
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-
-
additional information
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antibodies raised against the 130000 MW polypeptide of DNA ligase I specifically recognize this species in an immunoblot and inhibit only the activity of DNA ligase I
-
additional information
Tequatrovirus T4
-
not inhibited by pamidronate
-
additional information
Tequatrovirus T4
-
not inhibited by 2,4-diamino-7-dimethylamino-pyrimido[4,5-d]pyrimidine, trimethoprim, and methotrexate
-
additional information
Tequatrovirus T4
-
not inhibited by adenosine-5'-O-(P2,P3-hypo-P1-oxo)-triphosphate and adenosine-5'-O-(P2,P3-hypo-P1-thio)-triphosphate
-
additional information
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-
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additional information
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inhibited strongly by mismatches at the 3'-OH acceptor terminus
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